KOBE-2602
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- CAS号:
- 454453-49-7
- 英文名:
- kobe-2602
- 英文别名:
- CS-1280;kobe2602;kobe 2602;kobe-2602;kobe2602, >96%;Kobe 2602, >=98%;KOBE 2602; KOBE-2602;2-[2,6-Dinitro-4-(trifluoroMethyl)phenyl]-N-(4-fluorophenyl)hydrazinecarbothioaMide;Hydrazinecarbothioamide, 2-[2,6-dinitro-4-(trifluoromethyl)phenyl]-N-(4-fluorophenyl)-;H-Ras,Inhibitor,antiproliferative,Kobe-2602,carcinoma,Kobe 2602,Kobe2602,inhibit,Ras,Raf
- 中文名:
- KOBE-2602
- 中文别名:
- KOS2602,RAS抑制剂;H-RAS·GTP与C-RAF-1RBD结合抑制剂(KOBE2602);2-[2,6-二硝基-4-(三氟甲基)苯基]-N-(4-氟苯基)肼基硫代甲酰胺
- CBNumber:
- CB72667510
- 分子式:
- C14H9F4N5O4S
- 分子量:
- 419.31
- MOL File:
- 454453-49-7.mol
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KOBE-2602化学性质
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沸点:
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450.8±55.0 °C(Predicted)
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密度:
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1.691±0.06 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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insoluble in H2O; ≥17 mg/mL in DMSO; ≥17.53 mg/mL in EtOH with ultrasonic
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酸度系数(pKa):
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9.35±0.70(Predicted)
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形态:
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solid
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KOBE-2602性质、用途与生产工艺
Kobe2602是选择性Ras抑制剂，抑制H-Ras GTP与c-Raf-1结合，Ki值为149 μM。
| Target | Value |
Ras
()
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149 μM(Ki)
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Kobe2602 (2-20 μM; 1 hour) exhibits Ras-Raf-binding inhibition in NIH 3T3 cells.
Kobe2602 has IC
50
value of approximately 10 μM for the cellular Ras-Raf-binding inhibition.
Kobe2602 (20 μM) efficiently inhibits the phosphorylation of MEK and ERK, downstream kinases of Raf in NIH 3T3 cells transiently expressing H-Ras
G12V
.
Kobe2602 inhibits Ras⋅GTP but not Ras⋅GDP.
Kobe2602 (20 μM) inhibits the anchorage-dependent proliferation of H-rasG12V-transformed cells.
Cell Proliferation Assay
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Cell Line:
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H-ras
G12V
-transformed NIH 3T3 cells
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Concentration:
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20 μM
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Incubation Time:
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24 hours , 48 hours, 72 hours
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Result:
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Efficiently inhibited colony formation in soft agar in a dose-dependent manner.
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Western Blot Analysis
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Cell Line:
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NIH 3T3 cells
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Concentration:
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2 μM, 20 μM
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Incubation Time:
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1 hour
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Result:
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Effectively reduced the amount of c-Raf-1 associated with H-Ras
G12V
in NIH 3T3 cells in a dose-dependent manner, indicating the inhibition of the cellular activity of Ras.
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Kobe2602 (80 mg/kg; p.o.; five consecutive days per week, for 17 days) exhibits antitumor activity on a xenograft of human colon carcinoma SW480 cells carrying the K-ras
G12V
gene.
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Animal Model:
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Female athymic nude mice (6-8 wk old), with SW480 cells xenograft
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Dosage:
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80 mg/kg
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Administration:
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Oral administration, five consecutive days per week, for 17 days
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Result:
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Caused inhibition of the tumor growth.
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KOBE-2602
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/04/30 | S6527 | KOBE-2602
Kobe2602 | 454453-49-7 | 2mg | 877.29元 |
| 2024/04/30 | HY-15717 | KOBE-2602
Kobe2602 | 454453-49-7 | 10mM * 1mLin DMSO | 1155元 |
454453-49-7, KOBE-2602 相关搜索:
- Aromatics, Miscellaneous Reagents, Pharmaceuticals, Intermediates & Fine Chemicals
- Inhibitors
- 药靶配体
- 细胞生物学试剂
- 小分子抑制剂，天然产物
- 小分子抑制剂
- C14H9F4N5O4S
- KOS2602,RAS抑制剂
- H-RAS·GTP与C-RAF-1RBD结合抑制剂(KOBE2602)
- 2-[2,6-二硝基-4-(三氟甲基)苯基]-N-(4-氟苯基)肼基硫代甲酰胺
- 454453-49-7
- H-Ras,Inhibitor,antiproliferative,Kobe-2602,carcinoma,Kobe 2602,Kobe2602,inhibit,Ras,Raf
- Hydrazinecarbothioamide, 2-[2,6-dinitro-4-(trifluoromethyl)phenyl]-N-(4-fluorophenyl)-
- KOBE 2602; KOBE-2602
- CS-1280
- kobe2602, >96%
- Kobe 2602, >=98%
- kobe-2602 2-[2,6-Dinitro-4-(trifluoromethyl)phenyl]-N-(4-fluorophenyl)hydrazinecarbothioamide
- 2-[2,6-Dinitro-4-(trifluoroMethyl)phenyl]-N-(4-fluorophenyl)hydrazinecarbothioaMide
- kobe-2602
- kobe2602
- kobe 2602